CAS: 200124-22-7; (S)-2-((Tert-Butoxycarbonyl)Amino)-5-(3-((2,2,4,6,7-Pentamethyl-2,3-Dihydrobenzofuran-5-yl)Sulfonyl)Guanidino)Pentanoic Acid

该化合物是L-arginine的一种受保护的衍生物,广泛用于peptide合成.三丁基碳基(Boc)组保护α-氨组,而2,2,4,4,6,7-五-sulfonyl (Pbf)组保护链的瓜尼功能.这种化合物在固态peptide合成(SPPS)中特别宝贵,因为它在酸性条件下具有稳定性,并且与基于氟化物的战略相容性.Pbf组在温酸条件下提供选择性的去保护,最大限度地减少副作用.它的高度纯度和可靠性能使它成为建造复杂的peptide的首选,确保高效的结合和最小的种族化.适合需要精确的子结合的研究和工业应用.

结构式图片

相似化合物

186698-61-3 154445-77-9 187618-60-6

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CAS号24424-99-5 二碳酸二叔丁酯 | CAS号200115-86-2 N5-[[[(2,3-二氢-2...

合成工艺路线路线简述

    Boc-Arg(Pbf)-Oh置于水,Lithium Hydroxide体系中,用 四氢呋喃 用作溶剂,化学反应 3.0H,反应生成N-叔丁氧羰基-N'-(2,2,4,6,7-五甲基二氢苯并呋喃-5-磺酰基)-L-精氨酸
    参考文献:Triazole Groups As Biomimetic Amide Groups In Peptides Can Trigger Racemization
    标题:Triazole Groups As Biomimetic Amide Groups In Peptides Can Trigger Racemization
    摘要:
    Doi:10.24820/ark.5550190.P011.484

    海关参考信息

    专利信息


    专利号:WO-2023030277-A1
    优先权日:2021-08-30
    标 题:Method for fully liquid-phase synthesis of grnh nonapeptide amide analog
    发明人:SUN PENGCHENG; PAN JING; WU JUNYONG; TANG YONGBO; Du Yixiong; GUO LIN
    权利人:HUNAN MICRO PEPTIDE BIOMEDICAL CO LTD
    摘要:Provided is a method for fully liquid-phase synthesis of a GRnH nonapeptide amide analog, which belongs to the technical field of medicine synthesis. The method comprises respectively synthesizing a 'Trp-Ser-Tyr' fragment, an 'R-Leu' fragment, a 'Pyr-His' fragment and 'Arg-Pro-Hunan T', wherein, R = D-Ala (alarelin), D-Leu (leuprorelin), D-Trp (deslorelin) and D-His (histrelin), and obtaining the GRnH nonapeptide amide analog with high yield and high purity by means of a '3 +2 +2 +2' fragment condensation method. The synthesis method is environmentally friendly, mild, and free of any highly toxic and poisonable reagents. The cost is greatly reduced and the synthesis method is very suitable for large-scale production.

    专利号:US-2018265547-A1
    优先权日:2014-07-18
    标 题 :Z-selective olefin metathesis of peptides
    发明人:MANGOLD SHANE L; GRUBBS ROBERT H
    权利人:CALIFORNIA INST OF TECHN
    摘要:The invention relates generally to the synthesis of modified amino acids and modified peptides in the presence of cyclometalated catalysts. The invention has utility in the fields of catalysis, organic synthesis, polymer chemistry, and industrial and fine chemicals chemistry.

    专利号:WO-2013057186-A1
    优先权日:2011-10-19
    标题 :Photolabile linker for the synthesis of hydroxamic acids
    发明人:NIELSEN THOMAS E; QVORTRUP KATRINE
    权利人:UNIV DANMARKS TEKNISKE
    摘要:The present invention relates to a photolabile hydroxamate linker based on the o - nitroveratryl group and its application for multistep solid-phase synthesis and controlled photolytic release of hydroxamic acids. The invention provides a method for producing a solid support comprising a hydroxylamine - functionalized photolabile linker, and the so produced hydroxylamine - functionalized photolabile solid support. The invention further provides a method for synthesizing a one-bead-one compound library of hydroxamic acid derivatives on a photolabile linker, as well as a method for screening a library of hydroxamic acid derivatives.

    专利号:CN-103159819-A
    优先权日:2013-03-29
    标题 :Synthesis of a Cholesterol Derivative and Its Application in Gene Transfection

    专利号:ES-2616871-T3
    优先权日:2009-06-01
    标 题 :Synthesis of relaxin peptide

    专利号:US-12172946-B2
    优先权日:2019-01-07
    标题:Compound containing diphenylmethane structure and use thereof
    发明人:LIANG WEIZHOU; ZHENG QINGQUAN; TANG QI
    权利人:GUANGZHOU TROJAN PHARMATEC LTD
    摘要:A structure of the compound containing a diphenylmethane structure of the present invention is represented by General Formula (1). The compound containing a diphenylmethane structure of the present invention contains a hydroxyl group, an amino group, a substituted amino group, and an active group, and can be used as an amino acid or peptide C-terminal protection reagent. A peptide synthesis reaction using this protection carrier has a fast reaction speed and a high reagent utilization rate in a suitable solvent system; post-treatment is carried out by means of simple liquid-liquid extraction separation, i.e. effective purification can be carried out, and finally, a product with a high purity can be obtained; and during a synthesis process, the change in solubility is small and an operation process has a strong universality, and therefore, the present method can be developed into a universal production method.
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    主要参考文献

    [参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1144.

    合成参考文献


    参考文献:10.1038/srep25069
    摘要:Liu H, Chang H, Lv J, Jiang C, Li Z, Wang F, Wang H, Wang M, Liu C, Wang X, Shao N, He B, Shen W, Zhang Q, Cheng Y. Screening of efficient siRNA carriers in a library of surface-engineered dendrimers. Scientific Reports. 2016 Apr 28;6(1):25069. doi: 10.1038/srep25069.
    参考文献:10.1007/978-1-0716-0227-0_15
    摘要:Abdel-Aal AM, Raz R, Papageorgiou G, Offer J. Synthesis of Amide Backbone-Modified Peptides. Methods Mol Biol. 2020;2103():225–37. doi: 10.1007/978-1-0716-0227-0_15.
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